5-oxo-ETE [Ligand Id: 3391] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL18028 (5-Oxo-ETE)
  • 12S-LOX/Arachidonate 12-lipoxygenase in Human [ChEMBL: CHEMBL3687] [GtoPdb: 1387] [UniProtKB: P18054]
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  • 15-LOX-1/Arachidonate 15-lipoxygenase in Human [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050]
  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • 15-LOX-2/Arachidonate 15-lipoxygenase, type II in Human [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296]
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  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
12S-LOX/Arachidonate 12-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3687] [GtoPdb: 1387] [UniProtKB: P18054]
ChEMBL Inhibition of human platelet 12-lipoxygenase by UV-visible spectrophotometry B 4.82 pIC50 15000 nM IC50 Bioorg. Med. Chem. (2014) 22: 4293-4297 [PMID:24924423]
15-LOX-1/Arachidonate 15-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050]
ChEMBL Inhibition of human reticulocyte 15-lipoxygenase-1 by UV-visible spectrophotometry B 4.6 pIC50 >25000 nM IC50 Bioorg. Med. Chem. (2014) 22: 4293-4297 [PMID:24924423]
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL Inhibition of rabbit reticulocyte 15-LOX by UV-visible spectrophotometry B 4.6 pIC50 >25000 nM IC50 Bioorg. Med. Chem. (2014) 22: 4293-4297 [PMID:24924423]
15-LOX-2/Arachidonate 15-lipoxygenase, type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296]
ChEMBL Inhibition of human reticulocyte 15-lipoxygenase-2 by UV-visible spectrophotometry B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. (2014) 22: 4293-4297 [PMID:24924423]
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
ChEMBL In vitro inhibitory activity against 5-lipoxygenase from rat basophilic leukemia cells. B 4.74 pIC50 18000 nM IC50 J. Med. Chem. (1987) 30: 1177-1186 [PMID:3599023]
OXE receptor/Oxoeicosanoid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628461] [GtoPdb: 271] [UniProtKB: Q8TDS5]
ChEMBL Desensitization of 5-oxo-ETE receptor in indo-1-labeled human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization F 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1987-1990 [PMID:21377873]
ChEMBL Agonist activity at human PK-tagged OXER1 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation assay F 6.66 pEC50 220 nM EC50 Bioorg Med Chem (2018) 26: 3580-3587 [PMID:29866479]
ChEMBL Agonist activity at OXE receptor (unknown origin) expressed in HEK293 cells co-expressing Galpha subunit G16 assessed as calcium mobilization using Oregon Green 488 BAPTA-1/AM by fluorescence assay F 7.17 pEC50 67 nM EC50 MedChemComm (2012) 3: 195-198
ChEMBL Agonist activity at 5-oxo-ETE receptor in human neutrophils assessed as stimulation of ca2+ mobilization F 8.15 pEC50 7 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1857-1860 [PMID:21316960]
GtoPdb - - 8.5 pEC50 3.1 nM EC50 J Biol Chem (1995) 270: 15029-36 [PMID:7797484];
Prostaglandins Other Lipid Mediat (2009) 89: 98-104 [PMID:19450703];
J Pharmacol Exp Ther (2008) 325: 698-707 [PMID:18292294];
J Biol Chem (1998) 273: 32535-41 [PMID:9829988];
J Biol Chem (1992) 267: 19233-41 [PMID:1326548]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]